371980-98-2
Chemical Structure
SB-612111
- CAS No.: 371980-98-2
- Formula:C24H29Cl2NO
- Molecular Weight:418.40
IUPAC Name: (5S,7S)-7-((4-(2,6-dichlorophenyl)piperidin-1-yl)methyl)-1-methyl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ol
InChIKey: OHRDCQFCAWLDBP-SBUREZEXSA-N
SMILES: O[C@H]1C[C@@H](CN2CCC(C3=C(Cl)C=CC=C3Cl)CC2)CCC4=C(C)C=CC=C41
Biological Activity: SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].
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SB-612111 | SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model. | |||||||||||||||||||||
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References
- [1]. Paola F Zaratin, et al. Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).J Pharmacol Exp Ther. 2004 Feb;308(2):454-61. [Content Brief]
